Tacrolimus (Topical)

Tacrolimus ointment is indicated for short-term and intermittent long-term therapy in the treatment of patients with moderate to severe atopic dermatitis in whom the use of alternative, conventional therapies are deemed inadvisable because of potential risks, or in the treatment of patients who are not adequately responsive to or are intolerant of alternative, conventional therapies. Tacrolimus ointment is also indicated in other skin conditions such as chronic cutaneous graft-vs-host disease, hand and foot eczema, allergic contact dermatitis, vitiligo, psoriasis, lichen planus, facial lichen, vulvar lichen sclerosus, pyoderma gangrenosum, leg ulcers in rheumatoid arthritis, steroid-induced rosacea & alopecia areata, annular erythema, chronic actinic dermatitis and recalcitrant facial erythema.

Tacrolimus is a macroiide immunomodulator produced by fungus, Streptomyces tsukubaensis. It has been demonstrated that Tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of Tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This leads to a general decrease in the entire inflammatory cascade.

Use in adults: Apply a thin layer of Tacrolimus ointment onto the affected skin areas twice daily and rub in gently and completely. Treatment should be continued for one week after clearing of signs and symptoms of atopic dermatitis. The safety of Tacrolim ointment under occlusion which may promote systemic exposure has not been evaluated. Tacrolimus ointment should not be used with occlusive dressings.

Use in Children:

• Tacrolimus 0.03% ointment can be used in pediatric patients 2 years of age and older.
• Tacrolimus 0.1% ointment can be used in children 16 years of age and older.

Use in Elderly Patients: Patients >65 years old received Tacrolimus ointment in phase 3 studies. The adverse event profile for these patients was consistent with that for other adult patients.

Formal topical drug interaction studies with Tacrolimus ointment have not been conducted. The concomitant administration of known CYP3A4 inhibitors in patients with widespread and/or erythrodermic disease should be done with caution. Some examples of such drugs are erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers and cimetidine.

Tacrolimus ointment is contraindicated in patients with a history of hypersensitivity to Tacrolimus or any other component of the preparation.

Topically applied Tacrolimus ointment have very few and rare type of side-effects including skin burning, pruritus, flu-like symptoms, allergic reactions, skin erythema, skin infections, headache, etc.

Pregnancy Category C. There are no adequate and well-controlled studies of topically administered Tacrolimus in pregnant women. Although systemic absorption of Tacrolimus following topical applications of Tacrolimus ointment is minimal relative to systemic administration, it is known that Tacrolimus is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from Tacrolimus, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Cautions should be exercised while treatment with Tacrolimus ointment in patients with atopic dermatitis predisposed to superficial skin infections. The safety of Tacrolimus ointment has not been established in patients with generalized erythroderma.

Tacrolimus ointment is not for oral use. Accidental oral ingestion of Tacrolimus ointment may lead to adverse effects associated with systemic administration of Tacrolimus. If oral ingestion occurs, medical advice should be sought.

Drugs affecting the immune response.

Do not store above 30°C. Keep away from light and out of the reach of children.